46001-36-9Relevant articles and documents
Synthesis of palladium complexes with quinolino-based tridentate ligands and their applications for norbornene polymerization
Liu, Hui,Shi, Xiaochao,You, Fen,Yuan, Haibin
, (2020)
Palladium complexes bearing new tridentate quinolino-based [N?NNox] ligands were synthesized and tested for the polymerization of norbornene. Upon activation of MAO, all the palladium complexes showed high catalytic activities for th
Discovery of an Inhibitor of the Proteasome Subunit Rpn11
Perez, Christian,Li, Jing,Parlati, Francesco,Rouffet, Matthieu,Yuyong,Mackinnon, Andrew L.,Chou, Tsui-Fen,Deshaies, Raymond J.,Cohen, Seth M.
, p. 1343 - 1361 (2017/03/08)
The proteasome plays a crucial role in degradation of normal proteins that happen to be constitutively or inducibly unstable, and in this capacity it plays a regulatory role. Additionally, it degrades abnormal/damaged/mutant/misfolded proteins, which serves a quality-control function. Inhibitors of the proteasome have been validated in the treatment of multiple myeloma, with several FDA-approved therapeutics. Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. A fragment-based drug discovery (FBDD) approach was utilized to identify fragments with activity against Rpn11. Screening of a library of metal-binding pharmacophores (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value ~2.5 μM) displayed strong inhibition of Rpn11. Further synthetic elaboration of 8TQ yielded a small molecule compound (35, IC50 value ~400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation of tumor cells in culture.
COMPOSITIONS AND METHODS FOR JAMM PROTEIN INHIBITION
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Page/Page column 90, (2014/05/24)
Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed.